Novel tasquinimod analogs having novel anticancer activity

Project ID: TECH-2025-31

Background

Disruption of microtubules has dramatic effects on cell division due to the essential role they
play in conjunction with the mitotic spindles during this process. Molecules that disrupt microtubule
function are currently in widespread clinical use in cancer treatment. Taxanes, vinca alkaloids, and
epothilones are among the most commonly used anti-mitotic cancer drugs. However, anti-mitotics can have
significant dose-limiting toxicities. Therefore, more selectively active and less toxic molecules that disrupt
microtubule function are desired. There is a need for new and improved antimitotic compounds.

Invention Description

Researchers at the University of Toledo have developed analogs of Tasquinimod with novel mitotic arresting properties.

Applications

These novel antimitotic compounds have great potential use in cancer therapy, particularly for tumors resistant to conventional microtubule-targeting agents. The ability to disrupt spindle formation and prolong mitotic arrest makes it a strong candidate for further preclinical and clinical development.

Advantages

• Reduced tubulin regrowth
• Disrupt microtubule function through activation of spindle assembly checkpoint and mitotic arrest
• Robust cytotoxicity against various cancer cell lines with IC₅₀ ranging from (0.3-5.0 μM)
• Potentially novel mechanism of altering microtubule dynamics